are anthracyclines topoisomerase inhibitors?
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- [Molecular determinants of response to topoisomerase II inhibitors]. [Article in French] Lansiaux A(1), Pourquier P. Author information: (1)Centre Oscar Lambret, Université Lille Nord de France. a-Lansiaux@o-lambret.fr
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- Top2 have been used as targets for the development of anticancer drugs. These inhibitors include anthracyclines (doxorubcin, daunorubicin, epirubicin) and epipodophyllotoxins (etoposide), which are widely used in the clinic. These drugs poison Top2 by trapping the enzyme on its DNA cleavage sites, which results in irreversible double-strand breaks that are responsible for cell death.
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Topoisomerase inhibitor (June 2011). Topoisomerase inhibitors are agents designed to interfere with the action of topoisomerase enzymes (topoisomerase I and II), which are enzymes that control the changes in DNA structure by catalyzing the breaking and rejoining of the phosphodiester backbone of DNA strands during the normal cell cycle.opoisomerase inhibitors are often divided according to which type of enzyme it inhibits. 1  Topoisomerase I inhibitors: irinotecan, topotecan, camptothecin and lamellarin D all target type IB topoisomerases,
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- Aspirin and nonaspirin nonsteroidal antiinflammatory drugs (NSAIDsJ inhibit platelet. cyclooxygenase, thereby blocking the formation of thromboxane A2• These drugs produce. a systemic bleeding tendency by impairing thromboxane-dependent platelet aggregation. and consequently prolonging the bleeding time.
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Stereoselective synthesis of exocyclic allenes by double hydride reduction of 3-alkynyl-2-cycloalkenones title = Stereoselective synthesis of exocyclic allenes by double hydride reduction of 3-alkynyl-2-cycloalkenones, abstract = Exocyclic allene natural products and pharmaceutical agents are rare but interesting compounds: Fucoxanthin, grasshopper ketone, and analogues of prostacyclins, cephalosporins, antithrombic agents and sterol biosynthesis inhibitors are representative.
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Topiramate Linked With Increased Risk for Nephrolithiasis Topiramate Linked With Increased Risk for Nephrolithiasis. November 10, 2006 — Treatment with the antimigraine agent topiramate ( Topamax, Ortho-McNeil) caused metabolic changes favoring the formation of calcium phosphate kidney stones in 2 exploratory studies. The finding is from an article published in the October issue of the American Journal of Kidney Diseases.
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Regular ArticlePhosphodiesterase 4 Conformers: Preparation of Recombinant Enzymes and Assay for Inhibitors Their immediate action is terminated through the activity of phosphodiesterases, a diverse family of enzymes. This diversity has given rise to drug discovery opportunities, and assay technology is therefore of key importance. Inhibitors of the cyclic-AMP-specific phosphodiesterases (the PDE4 family) are drug candidates for a variety of inflammatory disorders. However, PDE4 inhibitors, besides their immunomodulatory effects, also cause side effects including nausea and emesis.
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ZEMPLAR CAPSULES Rx Potentiated by potent CYP3A4 inhibitors (eg, ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole); monitor and dose adjustment may be needed.
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Herbicide List of mechanisms found in modern herbicides. 1  ACCase inhibitors compounds kill grasses. 2  ALS inhibitors: the acetolactate synthase (ALS) enzyme (also known as acetohydroxyacid synthase, or AHAS) is the first step in the synthesis of the branched-chain amino acids (valine, leucine, and isoleucine).
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- Serrazimes-I shows in vitro activity similar to Serrapeptidase, but uses a protease system from Aspergillus melleus and Aspergillus oryzae. Like Serrapeptidase, protease from Aspergillus melleus has been shown both in vitro and in vivo to significantly inhibit inflammatory responses (Fossati, 2000).
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Antiprotozoal The mechanisms of antiprotozoal drugs differ significantly drug to drug. For example, it appears that eflornithine, a drug used to treat trypanosomiasis, inhibits ornithine decarboxylase, while the aminoglycoside antibiotic/antiprotozoals used to treat leishmaniasis are thought to inhibit protein synthesis.
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Protease inhibitor (pharmacology) Protease inhibitors (PIs) are a class of antiviral drugs that are widely used to treat HIV/AIDS and hepatitis C. Protease inhibitors prevent viral replication selectively binding to viral proteases (e.g. HIV-1 protease) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles.
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Types of Chemotherapy These drugs act during multiple phases of the cell cycle and are considered cell-cycle specific. There are several types of antitumor antibiotics: Anthracyclines: Doxorubicin, Daunorubicin, Epirubicin, Mitoxantrone, and Idarubicin. Chromomycins: Dactinomycin and Plicamycin.
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- Aspirin and nonaspirin nonsteroidal antiinflammatory drugs (NSAIDs) inhibit platelet cyclooxygenase, thereby blocking the formation of thromboxane A2. These drugs produce a systemic bleeding tendency by impairing thromboxane-dependent platelet aggregation and consequently prolonging the bleeding time.
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Aromatase Inhibitors Among postmenopausal women with hormone receptor-positive breast cancer, aromatase inhibitors (alone or after tamoxifen) offer the same or slightly greater benefit compared to tamoxifen alone [62,69-71]. Anastrozole, exemestane and letrozole are equally effective and have similar side effects [62,69-71].
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- In humans, inhibition of xanthine oxidase reduces the production of uric acid, and several medications that inhibit xanthine oxidase are indicated for treatment of hyperuricemia and related medical conditions including gout.Xanthine oxidase inhibitors are being investigated for management of reperfusion injury.urine analogues include allopurinol, oxypurinol, and tisopurine. Others include febuxostat, topiroxostat, and inositols (phytic acid and myo-inositol). In experiments, numerous natural products have been found to inhibit xanthine oxidase in vitro or in model animals (mice, rats).
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Topoisomerase Inhibitors Summary. 1  The nuclear enzymes topoisomerase I and II are critical for DNA function and cell survival, and recent studies have identified these enzymes as cellular targets for several clinically active anticancer drugs. Topoisomerase II inhibitors (anthracyclines, epipodophyllotoxins, etc.) are active against several types of tumours. However, treatment with these drugs often results in the development of the multi-drug resistance.
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- Angiotensin-Converting Enzyme (ACE) Inhibitors. 1  Commonly prescribed include: 2  Captopril (Capoten) 3  Enalapril (Vasotec) 4  Fosinopril (Monopril) 5  Lisinopril (Prinivil, Zestril) 6  Perindopril (Aceon) 7  Quinapril (Accupril) 8  Ramipril (Altace) 9  Trandolapril (Mavik)
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- Mechanism of Action. Ciclopirox is a hydroxypyridone antifungal agent that acts by chelation of polyvalent cations (Fe 3+ or A1 3+), resulting in the inhibition of the metal-dependent enzymes that are responsible for the degradation of peroxides within the fungal cell.
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Diagnosis These include antacids (Maalox, Mylanta, others); medications that reduce acid production, called H-2-receptor blockers, such as cimetidine (Tagamet HB) and ranitidine (Zantac); and medications that block acid production and heal the esophagus, called proton pump inhibitors, such as lansoprazole (Prevacid) and omeprazole (Prilosec).
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- Blood levels of cyclosporine, an immunomodulator, may be increased with concurrent use of omeprazole. Clopidogrel, a blood thinner, may not be activated properly if used concurrently with omeprazole. It may be best to use a different antacid.
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Chemotherapy Extravasation Doxorubicin and the other anthracycline vesicants (daunorubicin, epirubicin, idarubicin) cause cell death (necrosis) by binding to the DNA in healthy tissue cells when they extravasate. In addition, anthracyclines are not easily metabolized by the body; they can remain in the tissues for a substantial period of time.
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Effect of Bacillus anthracis virulence factors on human dendritic cell activation Studies point toward inhibition of multiple innate immune functions of several cell types by the three primary B. anthracis virulence factors—namely, capsule, LT, and ET. Among innate immune cells are DCs, which secrete cytokines in response to pathogen-associated molecular patterns (PAMPs) [30] .
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- Protease Inhibitors Nucleotide Reverse Agenerase ( generic name : amprenavir ) Transcriptase Inhibitor Crixivan ( indinavir ) Viread ( tenofovir , PMPA ) Fortovase ( saquinavir ) Kaletra ( lopinavir plus ritonavir ) Nucleoside Reverse Norvir ( ritonavir ) Transcriptase Inhibitors Viracept ( nelfinavir ) Combivir ( AZT plus 3TC ) Epivir ( lamivudine ...
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Antibiotics Used to Treat Staphylococcus Aureus The new class of drugs was known as beta-lactamase inhibitors and they worked to block the ability of the S. aureus bacteria to destroy the distinctive penicillin ring structure. The new combination drugs that are effective against Staphylococcus aureus infections are amoxicillin/clauvulante, ampicillin/sublactam, piperacillin/tazobactam and ticarcillin/clavulanate.
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Type II topoisomerase 1 Type IIA topoisomerases include the enzymes DNA gyrase, eukaryotic topoisomerase II (topo II), and bacterial topoisomerase IV (topo IV). 2  These enzymes span all domains of life and are essential for function.
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- In this study we examined the hemodynamic effects of methylene blue (MB), an inhibitor of guanylate cyclase, administered during cardiopulmonary bypass (CPB) to patients taking angiotensin-converting enzyme inhibitors.